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Terazosin | CAS No: 63590-64-7 | GMP-certified suppliers
A medication that treats symptomatic benign prostatic hyperplasia and hypertension by relaxing smooth muscle and reducing vascular resistance.
Therapeutic categories
Primary indications
- Terazosin is indicated for use in treating symptomatic benign prostatic hyperplasia and hypertension
Product Snapshot
- Terazosin is formulated as oral capsules and tablets, as well as ophthalmic solutions
- It is primarily utilized for the treatment of benign prostatic hyperplasia and hypertension
- Terazosin is approved for use in the United States and Canada markets
Clinical Overview
The mechanism of action involves antagonism of alpha-1 adrenergic receptors, which inhibits the vasoconstrictive effects of catecholamines such as adrenaline. This receptor blockade results in relaxation of smooth muscle in arterial walls and the prostate gland, leading to lowered peripheral vascular resistance and reduced urinary obstruction, respectively. The smooth muscle component constitutes approximately 40% of prostate volume; thus, its relaxation significantly decreases urethral pressure. Terazosin also modulates cellular processes by inhibiting catecholamine-induced mitogenesis and inducing apoptosis in prostate cells. This apoptotic effect is associated with increased expression of transforming growth factor beta-1 (TGF-beta1), upregulation of the cyclin-dependent kinase inhibitor p27kip1, and activation of caspase pathways.
Pharmacodynamically, terazosin’s alpha-1 receptor blockade contributes to its antihypertensive and urological actions. Pharmacokinetic data indicate oral bioavailability, with hepatic metabolism and renal elimination playing key roles in drug disposition. Terazosin interacts with P-glycoprotein transporters, which may influence absorption and distribution.
Safety considerations include potential adverse effects typical of alpha-1 blockers such as orthostatic hypotension, dizziness, and syncope, particularly after the initial dose or dosage escalation. Careful titration and monitoring are advised to mitigate hypotensive episodes. Terazosin is categorized under antihypertensive agents and drugs used in benign prostatic hyperplasia.
For pharmaceutical manufacturing and sourcing, the active pharmaceutical ingredient (API) Terazosin (CAS number 63590-64-7) must be obtained from suppliers complying with current Good Manufacturing Practice (cGMP) standards. Analytical characterization and stringent impurity profiling are essential to ensure consistent quality and regulatory compliance, especially for global distribution.
Identification & chemistry
| Generic name | Terazosin |
|---|---|
| Molecule type | Small molecule |
| CAS | 63590-64-7 |
| UNII | 8L5014XET7 |
| DrugBank ID | DB01162 |
Pharmacology
| Summary | Terazosin is a selective alpha-1 adrenergic receptor antagonist that induces relaxation of vascular and prostatic smooth muscle, leading to decreased blood pressure and improved urinary flow. Its pharmacological effects include inhibition of catecholamine-induced mitogenesis and promotion of apoptosis in prostate cells through upregulation of transforming growth factor beta-1 and activation of the caspase pathway. Terazosin primarily targets alpha-1A, alpha-1B, and alpha-1D adrenergic receptors and associated signaling pathways. |
|---|---|
| Mechanism of action | Terazosin is selective for alpha-1-adrenoceptors but not their individual subtypes. Inhibition of these alpha-1-adrenoceptors results in relaxation of smooth muscle in blood vessels and the prostate, lowering blood pressure and improving urinary flow. Smooth muscle cells accounts for roughly 40% of the volume of the prostate and so their relaxation reduces pressure on the urethra. It has also been shown that catecholamines induce factors responsible for mitogenesis and alpha-1-adrenergic receptor blockers inhibit this effect. A final long term mechanism of terazosin and other alpha-1-adrenergic receptor blockers is the induction of apoptosis of prostate cells. Treatment with terazosin enhances the expression of transforming growth factor beta-1 (TGF-beta1), which upregulates p27kip1, and the caspase cascade. |
| Pharmacodynamics | Terazosin is a quinazoline derivative alpha-1-selective adrenergic blocker. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Alpha-1A adrenergic receptor | Humans | antagonist |
| Alpha-1B adrenergic receptor | Humans | antagonist |
| Alpha-1D adrenergic receptor | Humans | antagonist |
ADME / PK
| Absorption | Approximately 90%. |
|---|---|
| Half-life | Terazosin has a mean half life 12 hours though this can be as high as 14 hours in patients over 70 years and as low as 11.4 hours in patients 20 to 39 years old. |
| Protein binding | 90-94%. |
| Metabolism | The majority of terazosin is hepatically metabolized. The metabolites recovered include 6-O-demethyl terazosin, 7-O-methyl terazosin, a piperozine derivative, and a diamine derivative. |
| Route of elimination | Approximately 10% of the oral dose is excreted unchanged in the urine and approximately 20% is excreted in the feces. 40% of the total dose is eliminated in urine and 60% of the total dose is eliminated in the feces. |
| Volume of distribution | 25L to 30L. |
| Clearance | Plasma clearance is 80mL/min and renal clearance is 10mL/min. |
Formulation & handling
- Terazosin is a small molecule primarily formulated for oral administration with available tablet, capsule, and liquid-filled capsule forms.
- The molecule has moderate water solubility (1.5 g/L) and logP (1.18), indicating balanced hydrophilicity and lipophilicity, suitable for oral delivery.
- Food intake does not significantly affect bioavailability but may delay peak plasma concentration by approximately 40 minutes; stability under standard handling conditions is expected given its small molecule nature.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient has patents that expired in the United States in 2010 and 2013, indicating a mature market with potential generic competition in both the US and Canada. Products containing this API are established in these markets. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | Terazosin is supplied by a broad range of generic manufacturers and packagers, indicating a well-established generic market. Branded products are present primarily in the US and Canadian markets. Given that relevant US patents expired in 2010 and 2013, generic competition is established and ongoing. |
|---|
Safety
| Toxicity | In the event of an overdose, patients may experience hypotension. Blood pressure and heart rate should be controlled by having the patient lie down or by treating with volume expanders or if necessary vasopressors. Patients should be monitored for renal function. Because terazosin is highly protein bound, dialysis is unlikely to provide benefit to overdosing patients. The oral LD50 in mice is 5500mg/kg[MSDS]. |
|---|
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- Terazosin exhibits high protein binding, reducing the efficacy of dialysis in overdose management
- 2
Terazosin is a type of Alpha blockers
Alpha blockers are a subcategory of pharmaceutical active pharmaceutical ingredients (APIs) that are widely used in the medical field. These medications are primarily utilized for their ability to block the alpha-adrenergic receptors, which are present in various parts of the body, including blood vessels and smooth muscle tissues. Alpha blockers work by preventing the receptor activation by the neurotransmitter norepinephrine, resulting in relaxation of the smooth muscles and dilation of the blood vessels.
These drugs find extensive applications in the treatment of several medical conditions. One of the most common applications of alpha blockers is in managing hypertension (high blood pressure) by promoting vasodilation, thereby reducing the resistance to blood flow. Additionally, they are employed in the treatment of benign prostatic hyperplasia (BPH) to relieve urinary symptoms by relaxing the smooth muscles in the prostate and bladder neck.
Some examples of popular alpha blockers include doxazosin, prazosin, and tamsulosin. Each of these medications may have specific indications and variations in their mechanism of action.
It is important to note that alpha blockers may cause certain side effects, such as dizziness, low blood pressure, and nasal congestion. Hence, it is crucial for healthcare professionals to carefully monitor patients receiving these medications and adjust the dosage accordingly.
In summary, alpha blockers are a vital subcategory of pharmaceutical APIs, playing a significant role in the management of conditions like hypertension and benign prostatic hyperplasia. Their mechanism of action involves blocking alpha-adrenergic receptors, leading to vasodilation and relaxation of smooth muscles. However, it is crucial to exercise caution while using these medications due to potential side effects.
Terazosin (Alpha blockers), classified under Antihypertensive agents
Antihypertensive agents are a crucial category of pharmaceutical active pharmaceutical ingredients (APIs) used to treat high blood pressure, also known as hypertension. These medications are designed to lower blood pressure and reduce the risk of associated cardiovascular complications.
Antihypertensive agents function by targeting various mechanisms involved in blood pressure regulation. Some common classes of antihypertensive agents include angiotensin-converting enzyme (ACE) inhibitors, angiotensin II receptor blockers (ARBs), beta-blockers, calcium channel blockers (CCBs), and diuretics.
ACE inhibitors work by inhibiting the enzyme responsible for converting angiotensin I to angiotensin II, a hormone that constricts blood vessels. ARBs, on the other hand, block the receptors to which angiotensin II binds, thereby preventing its vasoconstrictive effects.
Beta-blockers reduce blood pressure by blocking the effects of adrenaline and noradrenaline, which are responsible for increasing heart rate and constricting blood vessels. CCBs inhibit calcium from entering the smooth muscles of blood vessels, resulting in relaxation and vasodilation. Diuretics promote the elimination of excess fluid and sodium from the body, reducing blood volume and thereby lowering blood pressure.
Antihypertensive agents are typically prescribed based on the individual patient's condition and specific needs. They can be used alone or in combination to achieve optimal blood pressure control. It is important to note that antihypertensive agents should be taken regularly as prescribed by a healthcare professional and may require periodic monitoring to ensure their effectiveness and manage any potential side effects.
In summary, antihypertensive agents play a vital role in the management of hypertension by targeting various mechanisms involved in blood pressure regulation. These medications offer significant benefits in reducing the risk of cardiovascular complications associated with high blood pressure.
Terazosin API manufacturers & distributors
Compare qualified Terazosin API suppliers worldwide. We currently have 8 companies offering Terazosin API, with manufacturing taking place in 7 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Abbott Labs | Producer | United States | United States | CEP, CoA, GMP, KDMF | 4 products |
| Apollo Healthcare Resourc... | Distributor | Singapore | Singapore | BSE/TSE, CEP, CoA, EDMF/ASMF, FDA, GMP, ISO9001, JDMF, KDMF, MSDS, USDMF, WC | 200 products |
| Bioindustria | Producer | Italy | Italy | CoA, USDMF | 12 products |
| Chemische Fabrik Berg | Producer | Germany | Germany | CEP, CoA, FDA, GMP | 20 products |
| Global Pharma Tek | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, ISO9001, MSDS | 484 products |
| Signa | Producer | Mexico | Mexico | CoA, USDMF | 42 products |
| Synthokem Labs | Producer | India | India | CoA | 9 products |
| Tianjin Zhongrui | Producer | China | China | CoA, WC | 3 products |
When sending a request, specify which Terazosin API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
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